产品
编 号：F752732
分子式：C27H31FN10O2
分子量：546.6
分子式：C27H31FN10O2
分子量：546.6
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CAS No: 2436473-55-9
产品详情
生物活性：
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
体内研究：
RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner.Animal Model:Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells
Dosage:10 mg/kg, 20 mg/kg
Administration:p.o.; daily; for 10 days
Result:The tumor growth was remarkably suppressed.
体外研究：
The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667.
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
体内研究：
RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner.Animal Model:Immunodeficient nude/nude mice bearing KIF5B-RET Ba/F3 cells
Dosage:10 mg/kg, 20 mg/kg
Administration:p.o.; daily; for 10 days
Result:The tumor growth was remarkably suppressed.
体外研究：
The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667.
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